Orodispersive dosage forms containing droxidopa

Abstract

A rapidly-orodispersible tablet containing a porous, bound powder matrix containing droxidopa. The bound matrix contains an acidulant, particularly citric acid, to delay, reduce, or inhibit the coloration of droxidopa during stress storage conditions, and suppress the effect of glycerin on the coloration of droxidopa-containing tablets. The tablet can be dividable along a functional seam printed into the bound powder matrix, to divide the tablet into sub-dosage units of the same mass of droxidopa.

1 .- 30 . (canceled) 
     
     
         31 . A rapidly orodispersible tablet comprising a porous, bound powder matrix comprising up to about 80% droxidopa, up to about 5% of an acidulant, and a binder, wherein the droxidopa comprises particles of the droxidopa bound within the bound powder matrix by the binder, and has a porosity of about 30% to about 80%. 
     
     
         32 . The tablet according to  claim 31 , further comprising about 3% to about 35% of a disintegrant, wherein the bound powder matrix further comprises particles of the disintegrant. 
     
     
         33 . The tablet according to  claim 32 , wherein the disintegrant is selected from the group consisting of microcrystalline cellulose, cross-linked polyvinylpyrrolidone, croscarmellose, sodium starch glycolate, and a combination thereof. 
     
     
         34 . The tablet according to  claim 32  wherein the bound powder matrix further comprises particles of the binder. 
     
     
         35 . The tablet according to  claim 31  wherein the bound powder matrix further comprises particles of the binder. 
     
     
         36 . The tablet according to  claim 31 , wherein the tablet comprises up to about 2% citric acid. 
     
     
         37 . The tablet according to  claim 36 , further comprising up to about 5% glycerin. 
     
     
         38 . The tablet according to  claim 37 , wherein a mass ratio of the citric acid to the glycerin is from about 1:3 to about 1:6. 
     
     
         39 . The tablet according to  claim 31 , wherein a portion of the acidulent comprises particles of the acidulent distributed throughout the bound powder matrix. 
     
     
         40 . The tablet according to  claim 31  further comprising up to about 5% glycerin. 
     
     
         41 . The tablet according to  claim 31 , comprising 20% to 66% droxidopa. 
     
     
         42 . The tablet according to  claim 41 , containing 1 mg to about 5,000 mg droxidopa. 
     
     
         43 . The tablet according to  claim 42 , containing 100 mg to 1,800 mg droxidopa. 
     
     
         44 . The tablet according to  claim 31 , wherein at least a portion of the acidulant is molecularly dispersed throughout the bound matrix. 
     
     
         45 . The tablet according to  claim 31 , wherein the bound powder matrix comprises at least five layers of the bound powder matrix that are bonded together by the binder. 
     
     
         46 . The tablet according to  claim 45 , wherein the bound powder matrix has a porosity of about 5% to about 80%. 
     
     
         47 . The tablet according to  claim 31 , wherein the bound powder matrix has a hardness of at least 1 kp and disperses in 30 seconds or less in a volume of 30 ml or less of water or saliva. 
     
     
         48 . The tablet according to  claim 47 , wherein the citric acid particles have a D(90) value of 75 microns or less. 
     
     
         49 . The tablet according to  claim 48  further comprising up to about 5% glycerin. 
     
     
         50 . The tablet according to  claim 49 , wherein a mass ratio of the citric acid to the glycerin is from about 1:3 to about 1:6.